Aspalathin: a rare dietary dihydrochalcone from Aspalathus linearis (rooibos tea)


Aspalathin (2′,3,4,4′,6′-pentahydroxy-3′-C-β-D-glucopyranosyldihydrochalcone) is a natural C-linked glucosyl dihydrochalcone present in Aspalathus linearis (Burm.f.) R.Dahlgren (rooibos), a South African endemic plant, popularly consumed globally as a herbal tea. Aspalathin is reported to possess potent anti-oxidant properties that are believed to be responsible for the health benefits of rooibos. Other pharmacological properties ascribed to the molecule include antidiabetic, antimutagenic, anti-inflammatory, antithrombotic, and xanthine oxidase inhibitory activities. The role of aspalathin in limiting the progression of metabolic disorders and preventing diabetes-induced cardiovascular complications has been reported. The aforementioned potential health benefits of aspalathin have rendered it a popular natural ingredient that is incorporated in various nutraceutical and cosmeceutical products for protection against different conditions. Percutaneous permeation studies revealed some degree of absorption through the skin, supporting its use in cosmetic preparations. To perform an in-depth assessment of the scientific literature available on aspalathin, a bibliometric analysis was carried out on publications for the period 1965–2020, using the Scopus database. A total of 140 articles were retrieved, indicating that South African authors are major contributors to aspalathin research. The most common areas of investigation were identified as anti-oxidation, chemistry/chemical profiling, antidiabetic and anti-inflammatory activities. A comprehensive literature search showed that there are currently only two available reviews on aspalathin. Hence, the present review aims to explore the history and fill gaps with regards to collating aspects of the synthesis, quality control, metabolism and various biological activities of the molecule.

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2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)


Acetyl-CoA carboxylase


Adenosine diphosphate


Aflatoxin B1


Advanced glycation end product


Phosphorylation of AMP-activated protein kinase


Adenosine triphosphate


Aortic output


Aspalathin-rich rooibos extract






Area under the curve


Butylated hydroxyanisole


Butylated hydroxytoluene


Body weight


Cell adhesion molecules


Cecal ligation puncture


Carnitine palmitoyltransferase1


Diode array detection


2′,7′-Dichlorofluorescein diacetate


Deutschland, Denken, and Yoken


Density functional theory






Deoxyribonucleic acid






Dextran sodium sulfate


Endothelial cell protein C receptor


Fatty acid β-oxidation


Free fatty acid




Fasting plasma glucose


Ferric reducing antioxidant power


Fermented rooibos extract


Fourier Transform




Gallic acid equivalents


Glucose transporter


Glycogen phosphorylase


Green rooibos extract


Aspalathin-rich rooibos extract


Glycogen synthase




Oxidised glutathione


High glucose


Human sodium glucose co-transporter 2


High-performance liquid chromatography


Human umbilical vein endothelial cells


Heart weight to body weight



IC50 :

Half maximal inhibitory concentration


Intraperitoneal glucose tolerance test


Ischemia–reperfusion injury


5,5′,6,6′-Tetrachloro-1,1′,3,3′-tetraethylimidacarbocyanine iodide


Liquid chromatography-tandem mass spectrometry


Lipid hydroperoxide




Low-density lipoprotein




Madin-Darby canine kidney


Multiple reaction monitoring


3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide


Nicotinamide adenine dinucleotide phosphate


Normal glucose


Near infrared


Nuclear magnetic resonance




Oxygen radical absorbance capacity

pAMPK (Thr172):

Adenosine monophosphate-activated protein kinase threonine-172


Phosphatidylinositol 3-kinase


Apparent rate of permeability


Poly (adenosine diphosphate ribose) polymerase


Protein C


Polymerase chain reaction


Phosphoenolpyruvate carboxykinase




Pyrogallol red


Phenylpyruvic acid-2-O-β-D-glucoside


Fermented rooibos aqueous extract


Ribonucleic acid


Reactive oxygen species


Stearoyl-coenzyme A desaturase


Scrambled ribonucleic acid


Sodium glucose co-transporter


Small interfering nuclear factor erythroid 2-related factor 2


Superoxide dismutase


Search Tool for the Retrieval of Interacting Genes/Proteins




Total antioxidant capacity


Trolox equivalent




Thin-layer chromatography


Ultra performance liquid chromatography coupled to photodiode array detector


Trimethylsilyl trifluoromethanesulfonate




Uncoupling protein 2


Xanthine oxidase inhibition


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The work was financially supported by the National Research Foundation of South Africa and the South African Medical Research Council.

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Correspondence to Alvaro M. Viljoen.

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Chaudhary, S.K., Sandasi, M., Makolo, F. et al. Aspalathin: a rare dietary dihydrochalcone from Aspalathus linearis (rooibos tea). Phytochem Rev (2021).

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  • Aspalathin
  • Aspalathus linearis
  • Dihydrochalcone
  • Rooibos
  • Bibliometrics
  • Anti-oxidant